Reagent -

A High Sensitivity Assay for Kinetic Analysis of Kinases and ATPases Based on Measurement of ADP Accumulation

DiscoveRx has developed a unique assay technology based on an enzyme-coupled detection system that measures ADP accumulation which has been widely applied for kinetic studies of proteins that utilize ATP, GTP or UTP. The kinetic assay format offers a number of benefits for kinase and ATPase research in particular, including a broad tolerance to additives, no need for a modified substrate, the a...
A Wide Range of Compound Efficacies Revealed Using PathHunter® Arrestin Assays

DiscoveRx has developed a novel application of our established Enzyme Fragment Complementation (EFC) technology that allows us to monitor protein-protein interaction events in whole cells. Using this approach, we have designed the PathHunter^® Arrestin assay that monitors arrestin binding to activated GPCRs. The activity is subsequently detected with a single addition, HTS friendl...
ADP Hunter™ Plus: A Rapid, Quantitative HTS Assay for GDP and UDP

There are numerous assays available to measure the activity of enzymes involved in the transfer of a phosphate from ATP to a substrate macromolecule. However, there are only a few assays for enzymes that utilize other nucleotide triphosphates, opening opportunities to address pharmacologically relevant targets.
GTPases are a broad family of enzymes with a wide variety of activitie...
Application of the PathHunter® Protein Interaction Assay to Receptor Tyrosine Kinases (RTKs): Developing a Non-Antibody One-Step Cell-Based Kinase Activity

Kinase targets have been extensively studied in biochemical assays using purified protein fragments for the kinase and the substrate. However, there is an increasing need to understand how kinases function in the context of a whole cell assay. DiscoveRx has pioneered a protein interaction assay system using our established Enzyme Fragment Complementation (EFC) β-Galactosidase detection sys...
[User Manual] cAMP Hunter™ eXpress GPCR Assays

The cAMP Hunter eXpress GPCR Assay can be used for small or large molecules. The kits provide a robust, highly sensitive and easy-to-use assay for monitoring G-protein coupled receptor (GPCR) activation based on 3'-5'-cyclic adenosine monophosphate (cAMP) production in cells.
[User Manual] cAMP Hunter™ Gs and Gi Cell Lines

cAMP Hunter Cell Lines are non-force-coupled Gs and Gi stable clonal cell lines that expedite drug screening by providing robust responses, with accurate pharmacology. They provide the means for the measurement of an ubiquitous second messenger (cAMP) to determine the mechanism of action of ligands. Each cell line has been characterized for its appropriate GPCR...
Cell-Based Assays for G-Protein Independent Signaling Using Arrestin Binding and Endocytosis

GPCR activation results in G-protein dependent events such as second messenger signaling, as well as initiation of a host of cellular responses that regulate function and activate alternative pathways that are independent of G-protein activation. Recent studies have highlighted the importance of G-protein independent signaling in normal and pathogenic tissue physiology. Two of the w...
Dual Purpose Cell Lines for Analysis of GPCR/Arrestin Interaction using PathHunter® and Natural Gq-Coupling Using the Improved Calcium No-WashPLUS (CaNWPLUS) Kit

DiscoveRx has developed a panel of over 30 naturally Gq-coupled or dual coupled GPCR/Arrestin cell lines that can be used in screening and profiling applications for both arrestin biology and calcium based signaling. This presents a number of interesting use case scenarios, such as sequential monitoring of both readouts in a single screen, or use of the same cell line for analysis of bot...
[User Manual] EFC BlocDetect Kit

The EFC BlocDetect Kit is used to identify compounds that inhibit beta-galactosidase complementation or beta-galactosidase activity. As described below, beta-galactosidase complementation is DiscoveRx’s core technology for both cell-based as well as biochemical assays. The assay has been validated for use in both 96-well and 384-well microplate formats....
Faster Chemiluminescent cAMP Detection by HitHunter® cAMP XS+ on the SpectraMax L Luminescence Microplate Reader
Functional Receptor Tyrosine Kinase Assays for Antibody therapeutics Using PathHunter® Technology

Kinase targets have been extensively studied in biochemical assays using purified protein fragments for the kinase and the substrate. However, there is an increasing need to understand how kinases function in the context of a whole cell assay. DiscoveRx has pioneered a protein interaction detection system using well-established Enzyme Fragment Complementation (EFC) technology, by monitoring the...
Functional Whole-cell Assays for Tyrosine Phosphorylation Using PathHunter® Technology

Kinase targets have been extensively studied in biochemical assays using purified protein fragments for the kinase and the substrate. However, there is an increasing need to understand how kinases function in the context of a whole cell assay. DiscoveRx has pioneered a protein interaction detection system using well-established Enzyme Fragment Complementation (EFC) technology. We show here that...
HitHunter® cAMP and cAMP Hunter™ Cell Line: Your Solution for Use with High Serum Samples, Difficult Gi Targets and Identification of Allosteric Modulators

The cAMP detection technologies are widely used in high throughput screening (HTS) for measuring a functional response of a GPCR consequent to ligand-binding. However, a robust and sensitive cAMP detection platform that allows one to differentiate a full agonist from a partial agonist or an antagonist response from an inverse agonist response while also being able to identify allosteric compoun...
New Cell-Based Kinase Assays for TrkA and Other Receptor Tyrosine Kinases using PathHunter™ Protein-Protein Interaction Technology

The PathHunter™ technology from DiscoveRx is an adaptation of Enzyme Fragment Complementation (EFC) that provides a novel, generic cell-based assay format for detecting protein-protein interactions. This approach has enabled development of a number of new screening and profiling assays for targets that have been difficult to address in a cell-based assay. One such class of targets, the re...
New Momentum for Kinase Drug Discovery
Novel Trafficking Assays for Pharmacochaperone Discovery Using Enzyme Fragment Complementation

DiscoveRx^® has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation in an HTS friendly, cell-based format. This unique technology provide a basis for the generation of novel cellular assays for intractable targets, and simplify the detection of cellular s...
[User Manual] PathHunter® Cytosolic Tyrosine Kinase Activity Assay

PathHunter® Cytosolic Tyrosine Kinase (CTK) Activity Assays are functional cell-based assays used for identification, screening or profiling of small molecule inhibitors. These assays cannot be used for functional testing of biologics.
[User Manual] PathHunter® Activated GPCR Internalization Assay

PathHunter^® Activated GPCR Internalization Assays are non-imaging, non-antibody based chemiluminescent detection assays that provide a direct and quantitative measurement of internalized GPCRs localized to early endosomes. This allows the internalization of GPCRs to be quantitatively measured in live cells without the need for expensive microscop...
[User Manual] PathHunter® Detection Kit

The PathHunter Detection Kit is to be used with PathHunter Cell Lines or cell lines made with ProLabel/ProLink expression or cloning vectors. The kit is easy-to-use and has been successfully run in both 96-well and 384-well microplate format. The resulting signal is chemiluminescent and is read with any standard plate reader. PathHunter products utilize the Enz...
[User Manual] PathHunter® eXpress Activated GPCR Internalization Assay

PathHunter^® eXpress Activated GPCR Internalization Assays are ready to use complete kits that contain everything you need to measure arrestin bound internalized GPCRs in live cells without the hassle of using antibodies, radioactivity or elaborate imaging. The eXpress kits include single use vials of frozen cells stably expressing the GPCR of int...
[User Manual] PathHunter® eXpress Cytosolic Tyrosine Kinase Functional Assay Kit

PathHunter^® eXpress Cytosolic Tyrosine Kinase (CTK) Functional Assay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay for monitoring cytokine receptor activation or cytosolic tyrosine kinase inhibition. The eXpress kits contain everything needed for a complete CTK experiment including cells, detection reagents,...
[User Manual] PathHunter® eXpress Nuclear Hormone Receptor Assay Kit

PathHunter^® eXpress Nuclear Hormone Receptor (NHR) Functional Assay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay for monitoring NHR activation, translocation and recruitment of coactivator/corepressor proteins. The eXpress kits contains all the reagents needed for a complete NHR experiment including cells...
[User Manual] PathHunter® eXpress Receptor Tyrosine Kinase Functional Assay Kit

PathHunter^® eXpress Receptor Tyrosine Kinase (RTK) Functional Assay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay for monitoring receptor tyrosine kinase activation, phosphorylation and recruitment of SH2
[User Manual] PathHunter® eXpress Total GPCR Internalization Assay

PathHunter^® eXpress Total GPCR Internalization Assays are ready to use complete kits that contain everything you need to measure internalized GPCRs in live cells but without imaging, antibodies or radioactivity. The eXpress kits include single use vials of frozen cells stably expressing the GPCR of interest, optimized cell plating reagent, chemiluminescent detection reagents and ...
[User Manual] PathHunter® β-Arrestin eXpress GPCR Assay

PathHunter β-Arrestin cell lines are stable clonal cell lines that expedite drug discovery and development by providing robust response to over 90% of all known G-protein coupled receptor (GPCRs), with accurate pharmacology. This assay measures an essential pathway in GPCR activation, i.e., β-arrestin recruitment to activated GPCRs, enabling scientist...
[User Manual] PathHunter® GPCR Explorer Kit

PathHunter^® GPCR Explorer kits are a simple and easy-to-use method for building on-demand functional GPCR assays. Whether you have a panel of mutant GPCR cDNAs, a favorite ortholog GPCR or a GPCR heterodimer you’d like to funct...
[User Manual] PathHunter® Receptor Tyrosine Kinase Functional Assay

PathHunter Receptor Tyrosine Kinase (RTK) Functional Assays are functional cell-based assays used for identification, screening or profiling of agonists, small molecule inhibitors and therapeutic biologics (peptides, proteins and various types of antibodies). Additionally, they have non-R&D applications as bioassays for QC testing and testing for anti-drug ...
[User Manual] PathHunter® Total GPCR Internalization Assay

PathHunter^® Total GPCR Internalization Assays are non-imaging, non-antibody based chemiluminescent detection assays that provide a direct and quantitative measurement of internalized GPCRs localized in early endosomes. This allows the internalization of GPCRs to be quantitatively measured in live cells with-out the need for expensive microscopy. The PathHunter system combines eng...
PathHunter® Cell-Based Kinase Assays: A Portfolio of HTS-friendly Cytoplasmic or Receptor Tyrosine Kinase Assays for Small Molecule Inhibitors as well as Monoclonal Antibodies

Kinase therapeutics includes both monoclonal antibodies (mAbs) and small-molecule inhibitors. DiscoveRx’s PathHunter^® protein: protein interaction system uses well-established Enzyme Fragment Complementation (EFC) technology by monitoring interaction of target proteins with SH2 phosphotyrosine binding domains. We demonstrate application of PathHunter^® cell-ba...
[User Manual] PathHunter® EA Detection Kit

The PathHunter^® EA Detection Kit is used with PathHunter Cell Lines that express the Enzyme Acceptor (EA) fragment of beta-galactosidase, such as EA-Nuc, EA-Cyto, or EA-beta-Arrestin Parental Cell Lines. This detection reagent formulation includes ED reagent, a small ProLabel-type peptide that complements with EA during assay incubation. The as...
[User Manual] PathHunter® Flash Detection Kit

The PathHunter Flash Detection Kit is to be used with PathHunter Cell Lines or cell lines made with ProLabel®/ProLink™ expression or cloning vectors. The kit is easy-to-use and has been successfully run in both 96-well and 384-well microplate format. The resulting signal is chemiluminescent and is read with any standard plate reader.
[User Manual] PathHunter® ProLabel Detection Kit

The PathHunter^® ProLabel^® Detection Kit is for use with PathHunter Cell Lines expressing ProLabel (PL) or ProLink™ (PK) expression or cloning vectors. The kit measures the total amount of ProLabel- or ProLink-tagged protein expressed in cells. The assay can be used in both 96-well and 384-well ...
[DiscoverX/SGC Technology Symposium] - Profiling Compounds in Primary Human Cell BioMAP Systems for Drug Discovery and Therapeutic Development in Inflammation and Cancer
PathHunter® β-Arrestin Assays as a Universal Tool For Orphan GPCR Analysis

Orphan GPCRs continue to represent a target class with immense potential for the discovery of novel therapeutic compounds. In spite of the proven track record of GPCRs as druggable targets, over 100 non-odorant GPCRs remain to have their cognate ligands identified. Here we present the PathHunter^® Arrestin assay as a facile screening approach to orphan GPCR drug discovery. In this...
PathHunter® β-Arrestin Assays: Determination of Pharmacology Differences Between Human and Ortholog GPCRs

DiscoveRx previously introduced a protein-protein interaction system using enzyme fragment complementation that provides a robust, HTS friendly format for monitoring the interaction of activated GPCRs and β-arrestin. To date, DiscoveRx has applied this technology to generate over 170 pre-validated human cell lines. More recently, the coupling of mouse and rat GPCRs in the arrestin signalin...
[User Manual] ProLink™ Detection Kit

The ProLink™ Detection Kit, a member of the Synergy Product Line, is used to confirm expression of ProLink-tagged proteins. ProLink (PK or ED) is a component of DiscoveRx’s β-gal complementation technology and is used to engineer all PathHunter^® protein-protein interaction cell lines, including β-Arrestin GPCR cell lines, ...
Propelling GPCR drug discovery with innovative products and services
Ultrasensitive, 3456 or 1536-Well Miniaturization-Friendly Chemiluminescent Detection of PathHunter® Cell-Based GPCR and Kinase Assays

DiscoveRx's PathHunter^® platform is a simple, cell-based, chemiluminescent assay format that allows for screening large numbers of small molecules or hybridoma supernatants in a one-step, no-wash format making it both user-friendly and HTS-compatible. In this study, we demonstrate the 3456- and 1536-well application of DiscoveRx's PathHunter GPCR β-...
Utilization of PathHunter® Arrestin Cell Lines for Detection of Arrestin Biased Ligands and Compound Pharmacology Distinct from Second Messengers

DiscoveRx has developed a panel of over 120 characterized GPCR cell lines that monitor receptor activity using interaction with human β-Arrestin. These cell lines have numerous applications in both high throughput screening and downstream compound analysis, and have now been successfully adopted by a number of pharmaceutical and biotechnology companies. A relatively recent application for ...
Cell-based Receptor Tyrosine Kinase Screening Reloaded - Development of a new cellular assay system for a target protein so far resistent against HTS formats
Chemiluminescent cAMP Detection Using DiscoverX HitHunter® Kits Compared With TR-FRET Assays
Discovery of Novel G-Protein or Arrestin-Biased Ligands Using a Suite of GPCR Signaling Platforms

As more is learned about the intricacies of GPCR signaling, the harder it becomes to accurately describe ligand activity using a single functional readout. It is now well appreciated that GPCR activation results in G-protein dependent as well as G-protein independent signaling events such as β-arrestin recruitment and internalization. The complex relatio...
The Human Kinome

The Human Kinome is an artistic representation of the human kinome phylogenetic tree based on extensive published research and recently annotated to include lipid, atypical and clinically-relevant mutant kinases. For the eight protein kinase groups depicted in the main dendrog...
[User Manual] InCELL Hunter™ Bromodomain Cell-Based Assay

InCELL Hunter™ Bromodomain Cell-Based Assays, when used in conjunction with a InCELL Hunter Detection Kit (96-0002, 96-0002L or 96-0002XL), provides a cell based assay to look at protein stability upon compound binding. The assay described in this booklet have been validated for use in 384-well microplate formats.
[User Manual] Calcium No WashPLUS Assay Kit

The DiscoveRx Ca NW^PLUS Assay Kit provides a fast, reliable method for detection of changes in intracellular calcium. Cells expressing a receptor of interest that signals through calcium are pre-loaded with a calcium-sensitive dye and then treated...
Comprehensive analysis of kinase inhibitor selectivity

We tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are important exceptions to this trend. The data further illustrate that selective inhibitors have been developed against the majority of kinases targeted by ...
A Novel Assay Platform for the Detection of Kinase-Inhibitor Binding in Intact Mammalian Cells

Assays that directly detect compound binding inside cells can be of great utility in translating in vitro data to more biologically relevant models. However, these types of intracellular binding assays have not been possible so far. Cellular assays for serveral targets are limited to downstream activity-based readouts which can be difficult to develop, may not be proximal to the target, or may ...
scanKINETIC: A broadly applicable tool for the kinetic characterization of interactions between small molecule inhibitors and protein targets from the kinase and bromodomain families

Inhibitor association and dissociation kinetics can have important effects on a compound’s drug-like properties and in vitro, cellular, and in vivo behaviors. The association and dissociation rates for protein target-inhibitor complexes are variable and can be both inhibitor and protein-dependent. In addition, it is often important to classify inhibitors as being reversible or irreversibl...
BROMOscan high throughput, quantitative ligand binding assays identify best in class bromodomain inhibitors from a screen of mature compounds thought to specifically target other protein classes

Post-translationally appended acetyllysine marks on histone tails are key regulatory features of the epigenetic code. Bromodomains are “readers” of this specific lysine acetylation code, playing an important role in chromatin remodeling and regulation of gene expression. Bromodomains have emerged as an important new druggable target class in small-molecule inhibitor drug discovery, ...
Phenotypic Approaches Defining Toxicity Mechanisms

We have applied a panel of primary human cell-based in vitro systems (the BioMAP® systems platform) that model complex aspects of disease and tissue biology to investigate the biological mechanisms that underlie certain drug adverse effects. Here we present the analysis of several anti-inflammatory kinase inhibitors in development, including inhibitors of Jak kinase (tofacitinib) and syk ki...
Multi-Parameter GPCR Screening: An Essential Tool for Uncovering GPCR Mutant Phenotypes

The recent appreciation of functional selectivity/ligand bias in GPCR signaling has uncovered new opportunities for therapeutic discovery and continues to increase our understanding of compound function. We reasoned that since ligands and hence receptor conformation can differentially stimulate particular signaling pathways, variations in amino acid composition could similarly bias receptors an...
InCELL Hunter™: A Novel Cellular Assay Platform for the Direct Measurement of Compound Binding to Intracellular Targets in Intact Mammalian Cells

Assays that directly detect compound binding inside cells can be of great utility in translating in vitro data to more biologically relevant models. However, these types of intracellular binding assays have not been possible so far. Cellular assays for these targets are limited to downstream activity-based readouts which can be difficult to develop, may not be proximal to the target, or m...
BioSeek: Differentiating p38MAPK Inhibitors - Bridging the Gap from In Vitro to In Vivo

THE CHALLENGE
Our client, a global integrated pharmaceutical company, entered the lead optimization stage with three p38MAPK antagonists. All three compounds were competitive inhibitors for ATP binding and indicated to treat rheumatoid arthritis (RA). At the time the client approached BioSeek, data from biochemical p38MAPK assays and THP1 monocyte cell-line-based assays were generated but...
BioSeek: Economic Impact of BioMAP® Profiling - Bridging the Gap from In Vitro to In Vivo

CHALLENGE
The client identified a novel IL-17 inhibitor as its lead compound to treat an autoimmune disease. Specifically, it had identified the compound in a phenotypic screen of mouse cells and tested it in a rodent model for Collagen-Induced Arthritis. At this point, our client had collected valuable pre-clinical insights about the efficacy of the compound based on cellular and biochem...
BioSeek: Explaining a Clinical Adverse Event - Bridging the Gap from In Vitro to In Vivo

THE CHALLENGE
Our client, a global integrated pharmaceutical company, had completed Phase I studies with an investigative therapeutic, Drug A, for a cancer indication. In the Phase I study, a small number of patients experienced a specific serious adverse event (AE). This AE was correlated with the patients’ recent use of a second and unrelated therapeutic, Drug B. While Drug B was ...
BioSeek: Secondary Activity of an Adrenergic Receptor Antagonist Bridging the Gap from In Vitro to In Vivo

THE CHALLENGE
The client was a global pharmaceutical company interested in adding therapeutics for benign prostatic hyperplasia (BPH) to its development pipeline, searching for opportunities outside the currently approved classes of BPH drugs.

Certain adrenergic receptor (AR) antagonists were already marketed to treat the urinary retention symptoms of BPH. Additional observat...
Mix-and-Read Assays For Regulated Ubiquitination & Degradation of Proteins Using PathHunter® Technology

Ubiquitin-mediated degradation of signaling proteins is a primary means of signal regulation in a wide variety of cellular processes including inflammatory signaling, DNA damage responses, developmental pathways, and the cell cycle. However, observation of these events with the throughput necessary for modern drug discovery has been challenging. Numerous reporter proteins exist that can be used...
Novel Assays and Human Model Systems for Epigenetic Drug Discovery

Epigenetics can be defined as inheritable alterations in gene expression that arise independently of DNA sequence changes. Despite its relative infancy, the emergence of druggable targets that impact epigenetic signaling has the potential to serve as a new and exciting strategy to the treatment of human diseases including cancer, autoimmune and metabolic diseases.
At DiscoveRx, we have de...
A Novel Assay Platform for the Detection of Kinase-Inhibitor Binding in Intact Mammalian Cells

Assays that directly detect compound binding inside cells can be of great utility in translating in vitro data to more biologically relevant models. However, these types of intracellular binding assays have not been possible so far. Cellular assays for serveral targets are limited to downstream activity-based readouts which can be difficult to develop, may not be proximal to the target...
BROMOscan high throughput, quantitative ligand binding assays identify best in class bromodomain inhibitors from a screen of mature compounds thought to specifically target other protein classes

Post-translationally appended acetyl-lysine marks on histone tails are key regulatory features of the epigenetic code. Bromodomains are “readers” of this specific lysine acetylation code, playing an important role in chromatin remodeling and regulation of gene expression. Bromodomains have emerged as an important new druggable target class in small-molecule inhibitor drug discovery,...
Validated Cell-Based Assays for Rapid Screening and Functional Characterization of Therapeutic Monoclonal Antibodies

Monoclonal antibodies (MAbs) represent one of the fastest growing classes of biotherapeutic molecules today. While many technologies exist for generating and panning large collections of antibody fragments, there is a clear need for tools that can reliably detect both the binding and functional activity of a monoclonal antibody in a fast, reproducible and cost effective manner. This requires va...
The Human Bromodomain Family

Development of drugs that target epigenetic signaling mechanisms is a new and exciting strategy for the treatment of cancer. Epigenetic processes including chemical modifications to DNA and also to the histone proteins that package the DNA in chromatin play a central role in gene expression and regulation. One of the most frequently occurring modifications is...
[User Manual] PathHunter® Pathway Assay

PathHunter^® Pathway Assays, when used in conjunction with the respective detection kit (indicated in the target specific data sheet) provide a cell-based functional assay to study various protein activities in a cell. The assays described in this booklet have been validated for use in 384-well microplate formats.
[User Manual] PathHunter® ProLabel®/ProLink™ Detection Kit

The PathHunter ProLabel/ProLink Detection Kit is to be used with PathHunter Cell Lines or cell lines made with ProLabel/ProLink (PL/PK) expression or cloning vectors. The kit is easy-to-use and has been successfully run in both 96-well and 384-well microplate format. The resulting signal is chemiluminescent and is read with any standard plate reader.
[DiscoverX/SGC Technology Symposium] - Cracking the Histone Code? Development of small-molecule inhibitors of the bromodomain acetyl-lysine interaction
[DiscoverX/SGC Technology Symposium] - Epigenetic Target Identification for Musculoskeletal Disease
Validated Cell-Based Assays for Rapid Screening and Functional Characterization of Therapeutic Monoclonal Antibodies

Monoclonal antibodies (MAbs) represent one of the fastest growing classes of biotherapeutic molecules today. While many technologies exist for generating and panning large collections of antibody fragments, there is a clear need for tools that can reliably detect both the binding and functional activity of a monoclonal antibody in a fast, reproducible and cost effective manner. This requires va...
The BioMAP® Platform of Primary Human Cell Systems for Phenotypic Drug Discovery and Development – Lessons Learned

Presentation given on 28 October 2013 at CHI's Fast Congress on Phenotypic Drug Discovery, Cambridge, MA

Abstract
Phenotypic drug discovery (PDD) is a target agonistic approach using biological systems to screen for new drugs. Primary human cells are useful for PDD as they can be incorporated into high throughput assays but are more physiologically ...
Primary Human Cell BioMAP® Profiling of Methotrexate, Tocilizumab, Adalimumab, and Tofacitinib Reveals Different Mechanisms of Action With Distinct Phenotypic Signatures

Background/Purpose
Proinflammatory cytokines cause joint inflammation and destruction in rheumatoid arthritis (RA) as exemplified by the therapeutic success of inhibiting tumor necrosis factor alpha (TNFa) by adalimumab (ADA) and interleukin (IL)-6 receptor (IL-6R) by tocilizumab (TCZ). Such biologics and small molecule inhibitors, including methotrexate (MTX) and ...
BioMAP® Primary Human Cell Systems for Improving Drug Discovery and Development

Improving the safety of drug candidates that enter clinical development requires assays that are more predictive of human outcomes. The BioMAP platform uses human primary cells to model complex aspects of disease and tissue biology and can be applied to better understand biological mechanisms that underlie drug efficacy and safety. Here we test Ibrutinib, a BTK inhibitor recently ap...
Detection of Endogenous Ligand Bias: A Case Study Using the Chemokine Receptor Family

The pattern of intracellular signaling downstream of GPCR activation is now known to be specific to the ligand-receptor pair as opposed to an inherent, rigid property of the receptor. In a drug discovery setting, this property of GPCRs is now being exploited to develop designer molecules that have tailored intracellular responses. Although pathway bias is typically associated with synthetic mol...
Detection of Cytokine and Growth Factor Receptor Dimerization Using Enzyme Fragment Complementation

Ligand-induced receptor dimerization is the first functional step in receptor activation, representing the most proximal, functional read-out for receptor activation. For the majority of Receptor Tyrosine Kinases these are homomultimer events whereas for cytokine receptor and other cell surface kinases these are typically heteromultimeric events. Standard cellular protein interaction techniques...
Dual kinase/bromodomain inhibitors for rationally designed polypharmacology

Concomitant inhibition of multiple cancer-driving kinases is an established strategy to improve the durability of clinical responses to targeted therapies. The difficulty of discovering kinase inhibitors with an appropriate multi-target profile has, however, necessitated the application of combination therapies, which can pose significant clinical development challenges. Epigenetic reader domai...
Primary Human Cell BioMAP® Profiling of Methotrexate, Tocilizumab, Adalimumab, and Tofacitinib

Background/Purpose: Proinflammatory cytokines cause joint inflammation and destruction in rheumatoid
arthritis (RA) as exemplified by the therapeutic success of inhibiting tumor necrosis factor alpha (TNFa) by
adalimumab (ADA) and interleukin (IL)-6 receptor (IL-6R) by tocilizumab (TCZ). Such biologics and small
molecule inhibitors, including methotrexate (MTX) and the recentl...
Extracting Meaning from Complex Data: Predictive Models for Mechanism of Action Classification from Phenotypic Assay Data – Application to Phenotypic Drug Discovery

SLAS2014 presentation by Dr. Ellen Berg describing some of the challenges encounted in extracting meaningful data

Agenda slide

Problem
Drug discovery productivity is at an all time low
We are swimming in oceans of data
High throughput technologies
New assay models and platforms

Needed
...
[2013 Society of Toxicology Poster] - Phenotypic Approaches Defining Toxicity Mechanisms

Improving the safety of drug candidates that enter clinical development requires assays that are more predictive of human outcomes. The BioMAP® platform uses human primary cells to model complex aspects of disease and tissue biology and can be applied to better understand biological mechanisms that underlie drug adverse effects. Here we present the analysis of several anti-inflammatory kina...
[User Manual] PathHunter® Cytosolic Tyrosine Kinase Functional Assay

PathHunter® Cytosolic Tyrosine Kinase (CTK) Functional Assays are functional cell-based assays used for identification, screening or profiling of agonists, small molecule inhibitors and therapeutic biologics (peptides, proteins and various types of antibodies). Additionally, they have non-R&D applications as bioassays for QC testing and testing for anti...
[User Manual] PathHunter® Receptor Tyrosine Kinase Activity Assay

PathHunter Receptor Tyrosine Kinase (RTK) Activity Assays are functional cell-based assays used for identification, screening, or profiling of small molecule inhibitors. This assay format cannot be used for functional testing of biologics.
[User Manual] PathHunter® Receptor Tyrosine Kinase Internalization Assays

PathHunter^® Receptor Tyrosine Kinase (RTK) Internalization Assays are nonimaging, non-antibody based chemiluminescent detection assays that provide a direct and quantitative measurement of internalized RTKs localized to early
The application of EFC technology to study forward trafficking of GPCRs

DiscoveRx has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation in an HTS friendly, cell-based format. This unique technology provide a basis for the generation of novel cellular assays for intractable targets, and simplify the detection of cellular signaling events using a simple one-step chemil...
[User Manual] cAMP Hunter™ Exenatide Bioassay Kit

cAMP Hunter Exenatide Bioassay Kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study Exenatide potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qualifie...
Understanding Mechanisms of Drug-Induced Liver Injury Using Primary Human Cell and Co-culture Systems

Drug induced liver injury, in particular the idiosyncratic type (IDILI), is extremely difficult to identify before a compound reaches the later stages of drug development, often not being detected until the clinical trials or
Predicting Toxic and Therapeutic Mechanisms of the ToxCast Chemical Library by Phenotypic Screening

Addressing safety aspects of drugs and environmental chemicals relies extensively on animal testing. However the quantity of chemicals needing assessment and challenges of species extrapolation require development of alternative approaches...
In Vitro Bioactivity in ToxCast Assays for Fruit and Vegetable Extracts

The ToxCast and Tox21 programs have generated in vitro screening data for over 1000 chemicals to aid in hazard identification and setting chemical testing priorities. These data, together with high-throughput
Predictive Models for Mechanism-of-Action Classification of Chemicals Using Phenotypic Data

Introduction. There is increasing interest in applying in vitro methods to characterize the potential toxicity of drugs and chemicals. Methods that would allow automatic classification of in vitro activity profiles into mechanism classes could be helpful in prioritizing novel agents.
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Modelling the Host-‐Tumour Stromal and Vascular Microenvironments to Support Compound Screening and Therapeutic Development
[2014 AACR Poster] Detection of EGFR, HER2, HER3 and HER4 Hetero- and Homodimerization Using EFC-based Cellular Assays

Ligand-induced receptor dimerization is the first functional step in receptor activation, representing the most proximal, functional read-out for receptor activation. Here we present a novel application of the Enzyme Fragment Complementation system to monitor receptor-receptor interactions at the s...
[2014 AACR Poster] Dual kinase/bromodomain inhibitors for rationally designed polypharmacology

Concomitant inhibition of multiple cancer-driving kinases is an established strategy to improve the durability of clinical responses to targeted therapies. The difficulty of discovering kinase inhibitors with an appropriate multi-target profile has, however, necessitated the application of combination ther...
[2014 DDC Conference] Rational design of dual kinase-bromodomain inhibitors for therapeutic polypharmacology

We recently reported that several clinical kinase inhibitors also inhibit bromodomain epigenetic reader proteins with

therapeutically relevant potencies (Nat. Chem. Biol. (2014) doi: 10.1038/nchembio.1471). Nanomolar activity on BRD4 by BI-2536 and TG-101348, clinical PLK1 and JAK2/FLT3 kinase inhibitors, respectively, was particularly ...
[2014 PEGS Conference] Detection of EGFR, HER2, HER3 and HER4 Hetero- and Homodimerization Using EFC-based Cellular Assays

Ligand-induced receptor dimerization is the first functional step in receptor activation, representing the most proximal,

functional read-out for receptor activation. Here we present a novel application of the Enzyme Fragment Complementation system to monitor receptor-receptor interac...
[2014 PEGS Conference] Validated Bioassays for Potency, Stability and Lot Release Testing of Biopharmaceuticals

Biologics represents one of the fastest growing classes of biopharmaceutical molecules today. One of the major bottlenecks in the development of biologics is the lack of ready-to-use bioassays for potency, stability and lot release testing.
[2014 PEGS Conference] Development of Novel Cell-based Assays to Detect Neutralizing Antibodies to Therapeutic Biologics

Neutralizing antibodies (NAbs) to biological drugs may cause loss of therapeutic efficacy and in some cases, loss of endogenous protein function as well. Standard immunoassays can detect anti-drug antibodies, but cannot differentiate neutralizing
[User Manual] PathHunter® NHR Assay

Nuclear Hormone Receptor (NHR) activation is comprised of four steps: 1) ligand binding to the NHR, 2) nuclear translocation, 3) recruitment of a Steroid Receptor Coactivator Peptide (SRCP), and 4) transcriptional activation of target DNA sequence. P...
[User Manual] PathHunter® eXpress Dimerization Assay Kit

PathHunter^® eXpress Dimerization Assay Kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study receptor-receptor interactions at the cell surface. The eXpress kits contain all the reagents needed for a complete assay
[User Manual] PathHunter® eXpress Receptor Tyrosine Kinase Internalization Assay Kit

PathHunter^® eXpress Receptor Tyrosine Kinase (RTK) Internalization Assay kits provide a robust, highly sensitive and easy-to-use, cell-based assay for monitoring a direct and quantitative measurement of internalized RTKs localiz...
[User Manual] Native Calcium GPCR Assays

Native Calcium GPCR Assays provide a fast, reliable method for detection of changes in intracellular calcium. Cells expressing a receptor of interest that signals through calcium are pre-loaded with a calcium-sensitive dye and then treated with compound. Upon stimulation, the receptor signals release of intracellular calcium, which results in an increase of dye...
[2014 World Pharma Congress] Phenotypic Screening of Compounds and Drug Combinations in BioMAP® Oncology Systems Reveals Divergent Effects on Clinically-relevant Biomarkers

The tumor microenvironment consists of a complex array of interacting players including hyperproliferative malignant epithelial cells, stromal fi broblasts, activated vasculature, as well as polarized and suppressed immune cells. Understand...
[AOM_RA-Infl_Paris] BioMAP® Systems Integrate Human Biology and Drug Discovery To Enable The Development of Safer and More Effective Anti-inflammatory Therapies

Although biologics have demonstrated utility for treatment of rheumatoid arthritis, a significant proportion of patients fail to respond or develop dose-limiting side effects. This, together
[User Manual] PathHunter® Dimerization Assay

PathHunter^® Dimerization Assays provide a robust, highly sensitive and easy-to-use cell-based functional assay to study various protein activities in a cell. The assays allow for the monitoring of receptor-receptor interactions at the&...
Novel Trafficking Assays for Pharmacochaperone Discovery Using Enzyme Fragment Complementation

DiscoveRx^® has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation in an HTS friendly, cell-based format. This unique technology provides a basis for the generation of novel cellular assays for intractable targets, and simplify the detection of cellular ...
GLP1 NAb Assay: A Case Study for Simple, Serum-tolerant Cell-based Assays to Detect Neutralizing Antibodies to Biosimilar and Bioinnovator drugs

Neutralizing antibodies (NAbs) to biological drugs may cause loss of therapeutic effi cacy and in some cases, loss of endogenous protein function as well. Standard immunoassays can detect anti-drug antibodies, but cannot differentiate neutralizing
Development of Simple, Robust Bioassays for Biosimilar & Biobetter Development

One of the major bottlenecks in the development of biosimilars is the need for good bioassays to create potency, stability and neutralizing antibody (NAb) assays. Ideal bioassays need to refl ect the clinical mechanism of action (MOA) of the biopharmaceutical
[User Manual] PathHunter® eXpress Nuclear Translocation Assays

PathHunter^® eXpress Nuclear Translocation assay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay for monitoring target protein translocation into the nucleus upon activation of the pathway. The eXpress kits contain everything needed for a complete experiment including cells, detection reagents, media and plat...
[User Manual] PathHunter® eXpress Cytosolic Tyrosine Kinase Activity Assay Kit

PathHunter^® eXpress Cytosolic Tyrosine Kinase (CTK) Activity Assay Kits are cell-based assays used for the identification, screening or profiling of small molecule inhibitors. This assay format cannot be used for functional testing of biologics.
[2014 ACR Conference Poster] Analysis of Anakinra in Primary Human Cell Systems Reveals an In Vitro Signature for Skin-related Side Effects

The therapeutic options for treatment of rheumatic diseases have grown and now include a variety of inflammatory pathway inhibitors, with diverse mechanisms, but having both shared and unique side effects. Understanding side effect mechanis...
[2014 ACR Conference Poster] Profiling 14-3-3η in Human Primary Cell Based Disease Models Reveals a Unique Pro-Inflammatory Phenotypic Signature Consistent with RA-Inflammation Biology

14-3-3 proteins represent a highly conserved seven-member family of ubiquitously expressed intracellular chaperonins that perform a broad range of signaling functions. The 14-3-3 eta (η) protein is an emerging diagnostic and prognostic ...
[2014 FAST Conference Poster] Effects of Bromodomain Inhibitors on Renal and Pulmonary Fibrosis

Despite the broad range of potential treatment targets, an effective therapy does not exist for fibrosis or, for most other types of organ fibrosis. One explanation may relate to the fact that these cellular events are part of the normal wo...
[User Manual] HitHunter® cAMP Assay for Small Molecules

The HitHunter cAMP Assay for Small Molecules kits provide a robust, highly sensitive, and easy-to-use assay for monitoring G-protein coupled receptor (GPCR) activation based on 3'-5'-cyclic adenosine monophosphate (cAMP) production in cells. This kit is ideal for screening and profiling small molecules. For testing biologics samples (e.g. crude biologic...
[User Manual] HitHunter® cAMP Assay for Biologics

The HitHunter cAMP Assay for Biologics kits provide a robust, highly sensitive, and easy-to-use assay for monitoring G-protein coupled receptor (GPCR) activation based on 3'-5'-cyclic adenosine monophosphate (cAMP) production in cells. This kit is ideal for testing biologics samples (e.g. crude biologic samples in serum or plasma, purified or non-purifi...
[2015 SLAS Conference Poster] Interrogating Allosteric interactions Using Multiple Readouts for GPCRs

Compounds that bind to allosteric sites offer many benefits over those which interact orthosterically. These include enhanced specificity, ability to operate only on receptor activation and reduced risk of overdose. A number of allosteric compounds have been identified in multiple disease
[2015 SLAS Conference Poster] BioMAP® Human Primary Cell Systems for Improving Drug Discovery and Development

Improving the safety and efficacy of drug candidates that enter clinical development require assays that are more predictive of human outcomes. The BioMAP platform uses human primary cells to model complex aspects of disease and tissue biology and can be applied to better understand
[2015 SLAS Conference Poster] Novel Trafficking Assays for Pharmacochaperone Discovery Using Enzyme Fragment Complementation

DiscoveRx^® has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation in an HTS friendly, cell-based format. This unique technology provides a basis for the generation of novel cellular assays for...
Elucidating Mechanisms of Toxicity Using Phenotypic Data from Human Primary Cell Systems – a Chemical Biology Approach for Thrombosis-Related Side Effects

There is increasing interest in applying in vitro methods to characterize the potential toxicity of drugs and chemicals.While data-driven approaches to build predictive models can be helpful for risk assessment, the ability to inform an in depth underst...
Analysis of α-PD-1, α-PD-L1 and α-CTLA-4 Immune Checkpoint Antibodies in Human Primary Cell BioMAP Oncology Systems

1. Our goal is to develop more robust and physiologically relevant in vitro models of the host-tumor microenvironment

• Co-cultures of human primary fibroblasts or
Japanese BioMAP®システム基礎から臨床への架け橋

BioMAP システムとは、ヒトの疾患に限りなく近い微小環境のもとでの薬理反応を測定する試験化合物・物質のフェノタイプ（表現型）プロファイリング技術であります。各システムは、一連のヒトプライマリー細胞を用いて、臨床結果や論文上で報告されている直接疾患に関与しているタンパク質やサイトカイン等の発現レベルを測定するとこによって、各試験物質にユニークなタンパク質発現プロファイルを作製します。そ...
[2015 Bioassay Conference] Simple, Reproducible & Robust Bioassays in Cryopreserved Ready-To-Assay Format

Cell-based bioassays often pose a hurdle during a rapidly moving biologics development program. High standards for assay accuracy, precision, reproducibility and robustness are additionally put to the test by the use of continuous culture cells that can add to assay variability and increase the cost and complexity of each assay.

Advent of new technology platforms can enabl...
[2015 SOT Conference Poster] Elucidating Mechanisms of Cardiovascular Toxicity Using Phenotypic Data from BioMAP Human Primary Cell Systems

We are applying a chemical biology approach for elucidating potential toxicity mechanisms for thrombosis-related side effects in humans. In previous work with the EPA for the ToxCast™ program, it was observed that several classes of chemicals, including aryl hydrocarbon receptor (AhR) agonists...
[2015 NAb Conference Poster] Robust and Simple Potency and NAb Bioassays for Avastin® Biosimilar Development

One of the major bottlenecks in the development of biosimilars is the need for good bioassays to create potency,

stability and neutralizing antibody (NAb) assays. Ideal bioassays need to reflect the clinical mechanism of action

(MOA) of the originator drug and should be simple, precise, reproducible and robust. In additio...
Advances in tools to compare potency, efficacy, safety & quality of follow-on biologics or biosimilars

Regulatory authorities define biosimilars as drugs that are “highly similar” to or “interchangeable” with an approved biologic. The lack of a pre-defined path to demonstrate similarity leaves the burden of proof on the
Quantifying Signaling Bias: A Simple Approach to Quantify Functional Selectivity and Agonist Bias

Interest in GPCR ligand bias has increased in recent years due to evidence that positive and negative aspects of drug activity can be driven by differential pathway signaling. As a result it is possible to develop drugs with reduced side effects th...
Simple, Reproducible & Robust Bioassays In Cryopreserved Ready-To-Assay Format

Cell-based bioassays often pose a hurdle during a rapidly moving biologics development program. High standards for assay accuracy, precision, reproducibility and robustness are additionally put to the test by the use of continuous culture cells tha...
[2015 WCI Conference] Measuring Receptor Dimerization To Create Functional Cell-Based Assays for ~85% of the Interleukin Receptor Family

Ligand-induced receptor dimerization is the first functional step in receptor activation, representing the most proximal, functional read-out for receptor activation. It is well understood that the family of Interleukin receptors will dimerize with the other members of its family leading to a complicated signaling cascade that is critically involved in a vari...
A novel dye-free cytotoxicity assay to selectively measure target cell death in ADCC, CDC CAR-T or T-cell activation assays

Antibody-dependent cell-mediated cytotoxicity (ADCC) is the mechanism by which many Class I therapeutic antibodies, including rituximab and trastuzumab, achieve clinical effi cacy. In particular, molecules based on IgG1 isotype may be expec...
Japanese Cell-Based Assays for Biologics
Japanese Enzyme Fragment Complementation (EFC) Overview
Japanese KINOMEscan Technology Platform
Japanese GPCR Technology Platform Overview
[User Manual] PathHunter® GPCR Bioassay Kit

PathHunter^® GPCR Bioassay kits are ready to use kits that contain everything necessary to perform a functional assay with live cells, without any continuous cell culture. This kit has been designed to rapidly detect the potency of your biologic or the presence of neutralizing antibodies against the biologic. The Bioassay kits include single use v...
[User Manual] cAMP Hunter™ GPCR Bioassay Kit

The cAMP Hunter™ GPCR Bioassay Kits provide a robust, highly sensitive and easy-to-use assay for monitoring G-protein coupled receptor (GPCR) activation based on 3'-5'-cyclic adenosine monophosphate (cAMP) production in cells.
[User Manual] PathHunter® Cytokine Receptor Bioassay Kit

<div style="text-align: justify;"> PathHunter Cytokine Receptor Bioassay kits are ready to use kits that contain everything necessary to perform a functional assay with live cells, without any cell culture. This kit has been designed to rapidly detect the efficacy of your biologic or the presence of neutralizing antibodies against the biologic. The bioassay kits include single use vials ...
[User Manual] PathHunter® Receptor Tyrosine Kinase Bioassay Kit

PathHunter® RTK (Receptor Tyrosine Kinase) Bioassay Kits are ready to use kits that contain everything to perform a functional assay with live cells, without any cell culture. This kit has been designed to rapidly detect the efficacy of your biologic or presence of neutralizing antibodies against the biologic. The bioassay kits include single use vials of f...
[User Manual] PathHunter® Dimerization Bioassay Kit

PathHunter^® Dimerization Bioassay Kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study receptor-receptor interactions at the cell surface. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay ...
[User Manual] PathHunter® Darbepoetin Alfa Bioassay Kit

PathHunter^® Darbepoetin Alfa Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study darbepoetin alfa potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and ...
[User Manual] PathHunter® Human Growth Hormone Bioassay Kit

PathHunter® Human Growth Hormone (hGH) Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study hGH potency and neutralizing antibodies. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, dilution buffer, and...
[User Manual] PathHunter® Insulin Lispro Bioassay Kit

PathHunter^® Insulin Lispro Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study insulin lispro potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, dilution b...
[User Manual] PathHunter® Aflibercept Bioassay Kit

PathHunter^® Aflibercept Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study aflibercept potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates...
[User Manual] PathHunter® Ranibizumab Bioassay Kit

PathHunter Ranibizumab Bioassay kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study ranibizumab potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-valid...
[2015 WCI Conference] Predicting Drug-induced Skin Rash Using BioMAP Human Primary Cell-based Systems

The relationship between drug efficacy and adverse events (AE) is dependent on (i) target selectivity, (ii) primary and secondary effects of target modulation and (iii) the concentration at which these interactions occur. BioMAP technology uses a systems biology approach to capture the complexity of physiologically relevant tissue microenvironments and ...
[2015 WCI Conference] Identiﬁcation of Immunomodulatory and Anti-Fibrotic Actions of Nintedanib and Pirfenidone Using BioMAP® Human Primary Cell-based Disease Models
Elucidating Mechanisms of Toxicity Using Human Primary Cell Systems

Purpose: Our goal is to identify in vitro assays that can predict adverse effects in humans and help elucidate mechanisms of toxicity. We performed large scale screening of approved drugs and experimental chemicals across panels of human primary cell based assays and co-cultures to identify assay endpoints that may be associated with particular adverse drug r...
Novel Trafficking Assays For Pharmacochaperone Discovery Using Enzyme Fragment Complementation Applied To CFTR-ΔF508

DiscoveRx^® has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation in an HTS friendly, cell-based format. This unique technology provides a basis for the generation of novel cellular assays for intractable targets, and simplify the detection of cellular ...
Quantifying Signaling Bias: A Simple Approach to Quantify Functional Selectivity and Agonist Bias

Interest in GPCR ligand bias has increased in recent years due to evidence that positive and negative aspects of drug activity can be driven by differential pathway signaling. As a result it is possible to develop drugs with reduced side effects that enhance positive effects through favoring one pathway over another. The availability of assays that can measur...
[User Manual] KILR® Assay for Suspension Cell Lines

The KILR cytotoxicity cell line enables the development of a simple, non-radioactive and dye-free method to specifically measure target cell death in a co-culture. The KILR assay has several applications in iOnc drug development including measuring target cell death through Antibody Dependent Cell-mediated Cytotoxicity (ADCC), Complement Dependent Cytotoxicity ...
[User Manual] KILR® Cytotoxicity Assay−Adherent Target Cell Lines

The KILR cytotoxicity cell line enables the development of a simple, non-radioactive and dye-free method to specifically measure target cell death in a co-culture. The KILR assay has several applications in Cancer Immunotherapy (iOnc) drug development including measuring target cell death through Antibody-Dependent Cell-mediated Cytotoxicity, ADCC, Complement-D...
[User Manual] PathHunter® Bioassay ED Detection Kit

The PathHunter Bioassay ED Detection Kit is to be used with PathHunter Bioassays cells overexpressing ProLabel®/ ProLink™-tagged (PL/PK-tagged) reporter or target proteins, but not expressing any EA. The Bioassay ED Detection reagent itself contains the complementary EA fragment. The kit is easy-to-use and can be run in both 96-well and 384-well micro...
[User Manual] PathHunter® Exendin-4 Bioassay Kit

PathHunter^® Exendin-4 Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study exendin-4 potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. Th...
[2015 BEBPA Conference Poster] Ready-to-use potency assays for anti-VEGF drugs like Bevacizumab

Cell-based bioassays often pose a hurdle during a rapidly moving biologics development program. High standards for assay accuracy, precision, reproducibility and robustness are additionally put to the test by the use of continuous culture cells that can add to variability and increase the cost and complexity of each assay. This is particularly challenging for...
[2015 BEBPA Conference Poster] Rapidly Develop Simple Potency Assays for Interleukins & Their Receptors

Ligand-induced receptor dimerization is an early functional step in receptor activation, representing the most proximal, functional read-out for Interleukin receptors. It is well understood that the family of Interleukin receptors will dimerize with the other members of its family leading to a complicated signaling cascade that is critically involved in a var...
[2016 SLAS Conference Poster] Improved Cell-Based Assays To Assess Therapeutic Molecules Against Immune Checkpoint Receptors Such As PD-1, PD-L1 and PD-L2

Regulation of immune responses is tightly controlled through a balance of co-stimulatory and inhibitory checkpoint receptors, often exploited by many cancers. Therefore, therapeutics that block inhibitory receptors have proved to be powerful agents to restore anti-tumor immune responses. One key inhibitory checkpoint receptor that is the target of sev...
[2016 SLAS Conference Poster] Phenotypic Characterization of CFTR Drugs, VX-770 and VX-809, in BioMAP® Human Primary Cell Systems Connects Target Biology to Disease Mechanisms

Cystic fibrosis (CF) patients have mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel that result in reduced membrane expression and function. CF patients have impaired lung function due to chronic airway inflammation driven by dysregulated Th17 and Th2 immune responses. These responses lead to overproduction of mucou...
[User Manual] PathHunter® IL1RL1/IL1RAP Dimerization Bioassay Kit

PathHunter^® IL1RL1/IL1RAP Dimerization Bioassay Kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study receptor-receptor interactions at the cell surface. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist...
[2016 Biopharmaceutical Symposium] Ready-to-use potency assays for anti-VEGF drugs such as Bevacizumab

Cell-based bioassays often pose a hurdle during a rapidly moving biologics development program. High standards for assay accuracy, precision, reproducibility and robustness are additionally put to the test by the use of continuous culture cells that can add to variability and increase the cost and complexity of each assay. This is particularly challenging for...
[User Manual] KILR® Retroparticles For Cytotoxicity Assays

The KILR Retroparticles provide a potent vehicle for the stable delivery of the KILR reporter construct into almost any dividing cell line, enabling the creation of KILR cytotoxicity assays in the cell line expressing the target of your choice. The KILR Cytotoxicity cell line you generate enables the development of a simple, non-radioactive and dye-free method ...
Improved Cell-Based Assays To Assess Therapeutic Molecules Against Immune Checkpoint Receptors Such As PD-1, PD-L1 And PD-L2

Regulation of immune responses is tightly controlled through a balance of co-stimulatory and inhibitory checkpoint receptors, often exploited by many cancers. Therefore, therapeutics that block inhibitory receptors have proved to be powerful agents to restore anti-tumor immune responses. One key inhibitory checkpoint receptor that is the target of several the...
Phenotypic Human Primary Cell-based Tumor Microenvironment Models for Evaluation of Drug Combinations for Immune Oncology

We have developed complex in vitro co-cultures of human primary cells to model disease states in a standardized format to enable phenotypic drug screening.

The Diversity PLUS panel of 12 BioMAP systems has been validated to test agents and combinations with respect to predicting efficacy and safety.

Additional panels relevant...
[2016 PEGS Conference] Specifically Measure Target Cell Death in a Co-Culture with Immune Cells Through a Non-Radioactive, Dye-free Cytotoxicity

Following the recent regulatory approvals of a number of checkpoint inhibitor therapeutics, development of a wide array of immunomodulatory therapeutic antibodies targeting novel antigens and with distinct mechanisms of action (MOA) have emerged. These include classical monoclonal antibodies, but also increasingly bi- and multi-specific antibodies designed to...
[2016 PEGS Conference] Novel, Improved Cell-based Assays to Enable Immunotherapy Drug Development for Checkpoint Receptors

Regulation of immune responses is tightly controlled through a balance of co-stimulatory and inhibitory checkpoint receptors, often exploited by many cancers. Therefore, therapeutics that block inhibitory receptors or activate immunostimulatory checkpoint receptors have proved to be powerful agents to restore anti-tumor immune responses. However, developing d...
[User Manual] PathHunter eXpress HEK 293 IkB Degradation Assays

PathHunter eXpress Pathway assay kits provide a robust, highly sensitive and easy-to-use method cell-based functional assay for IκB degradation and NFκB pathway activation. The eXpress kits contain everything needed for a complete IκB degradation assay including cells, detection reagents, media, and plates. The prevalidated, frozen eXpress cel...
[User Manual] PathHunter® β-Arrestin2 Retroparticles

The PathHunter β-Arrestin2 Retroparticles includes Moloney murine leukemia retrovirus (MMLV) expressing β-arrestin2 fused to the β-galactosidase (β-gal) reporter fragment called EA (enzyme acceptor). The Retroparticles can be used for effective transduction of a wide variety of dividing target cells (e.g. CHO, HEK 293, U2OS) resulting in hig...
Phenotypic Profiling in BioMAP® Human Primary Cell Systems Identifies a Tox Alert Signature for Skin Irritation

Rationale. We have elucidated toxicity mechanisms of known adverse effects (AEs) associated with clinical drugs using a chemical approach in our BioMAP human primary cell-based systems modeling human tissue and disease. In previous work with the Environmental Protection Agency’s (EPA) ToxCast™ program and in downstream studies, we tested compounds...
[User Manual] PathHunter® EA Parental Cell Lines

The PathHunter EA Parental Cell Lines are engineered cell lines that stably express a particular reporter protein fused to a large β–galactosidase (β-gal) enzyme reporter fragment called EA (enzyme acceptor). The EA parental cell lines have various cell backgrounds and are intended to be used with ProLabel®/ ProLink™-tagged proteins to...
[User Manual] PathHunter® TrkC Bioassay Kit

PathHunter^® TrkC Bioassay kits provide a robust, highly sensitive, and easy-to-use, cell-based functional assay to study potency of drugs targeting Neurotrophin 3 or the TrkC receptor. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, dilut...
[User Manual] PathHunter® IGF1R Bioassay Kit

PathHunter IGF1R Bioassay kits provide a robust, highly sensitive, and easy-to-use, cell-based functional assay to study potency of drugs targeting IGF1, IGF2, or the IGF1 receptor. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, dilution buffer, and assa...
[2016 XXIV National Medicinal Chemistry] Interrogating Allosteric Interactions Using Multiple Readouts for GPCRs

Compounds that bind to allosteric sites offer many benefits over those which interact orthosterically. These include enhanced specificity, ability to operate only on receptor activation and reduced risk of overdose. A number of allosteric compounds have been identified in multiple disease areas including CNS (physiological and neuropathic disorders), metaboli...
[User Manual] PathHunter® Checkpoint Signaling Assay - Immunoglobulin Superfamily (IgSF)

The PathHunter Checkpoint Receptor Signaling Assay is a simple, highly specific assay to enable discovery and development of small molecule and biologic drugs targeting immune checkpoint receptors, belonging to the Immunoglobulin Superfamily (IgSF), such as PD-1, CD28 and ICOS.
[User Manual] cAMP Hunter™ Follitropin Alfa Bioassay Kit

cAMP Hunter Follitropin Alfa Bioassay Kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study potency and neutralizing antibodies for Follitropin Alfa and its analogues. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist...
[User Manual] PathHunter® Bioassay Detection Kit

The PathHunter Bioassay Detection Kit is to be used with PathHunter Bioassay cells or PathHunter Cell Lines. The kit is easy-to-use and has been successfully run in a 96-well microplate format. The resulting signal is chemiluminescent and is read with any standard plate reader.
[User Manual] PathHunter® Panitumumab Bioassay Kit

PathHunter Panitumumab Bioassay kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study panitumumab potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-valid...
[User Manual] InCELL Detection Kit

The InCELL Detection Kit is to be used with InCELL Pulse assays made with ProLabel expression or cloning vectors. This kit has a 96-well plate format, is easy-to-use, and results in a chemiluminescent signal that can be read with any standard plate reader.
[User Manual] InCELL Pulse™ Cellular Target Engagement Assays

InCELL Pulse Cellular Target Engagement Assays are 96-well plate format kits for the assessment of inhibitor cellular potency. The assay uses DiscoverX’s proprietary enzyme fragment complementation (EFC) technology to measure compound-dependent thermal stabilization of target proteins in a cellular context. InCELL Pulse enables the measurement of quantita...
[User Manual] PathHunter® eXpress Receptor Tyrosine Kinase Activity Assay Kit

PathHunter^® eXpress Receptor Tyrosine Kinase (RTK) Activity Assay Kits are functional cell-based assays used for identification, screening or profiling of small molecule inhibitors. This assay format cannot be used for functional testing of biologics.
[User Manual] ProLabel® and ProLink™ Mammalian Cloning Vectors

pCMV Mammalian cloning vectors are intended for cloning your protein of interest (e.g. membrane protein or intracellular protein) with ePL, PK1 or PK2, as a N- or C-terminal tag, and subsequently transfecting into a parental cell line expressing an EA-tagged reporter protein (Note: in some assay formats the cells only express an ED protein and the EA protein is...
[User Manual] cAMP Hunter™ Teriparatide Bioassay Kit

cAMP Hunter Teriparatide Bioassay Kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study Teriparatide potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qu...
[User Manual] PathHunter® PTH Bioassay Kit

PathHunter^® Parathyroid Hormone (PTH) Bioassay kits are ready to use kits that contain everything necessary to perform a functional assay with live cells, without any continuous cell culture. This kit has been designed to rapidly detect the potency of your biologic or the presence of neutralizing antibodies against the biologic. The Bioassay ki...
[User Manual] InCELL Hunter™ Target Engagement Assay Kit

The InCELL Hunter™ Target Engagement Assay Kit provides a simple and easy-to-use method for building on-demand intracellular binding assays. This unique platform allows rapid generation of cell-based assays that measure quantitative changes in protein stability upon compound binding. Whether you are studying intracellular protein or lipid kinases, phospho...
[User Manual] PathHunter® IL-2 Bioassay Kit

PathHunter^®IL-2 Bioassay kits provide a robust, highly sensitive, and easy-to-use cell-based functional assay to study IL-2 potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre...
[User Manual] PathHunter® Epoetin Alfa Bioassay Kit

PathHunter^® Epoetin Alfa Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study epoetin alfa potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, an...
[User Manual] PathHunter® GLP1 (7-37) Bioassay Kit

PathHunter^® GLP1 (7-37) Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study GLP1 (7-37) potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plat...
[User Manual] PathHunter® Bevacizumab Bioassay Kit

PathHunter^® Bevacizumab Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study bevacizumab potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates...
[User Manual] PathHunter® β-Arrestin Assay for GPCR Cell Lines

PathHunter β-Arrestin cell lines are stable clonal cell lines that expedite drug discovery and development by providing robust response to over 90% of all known G-protein coupled receptor (GPCRs), with accurate pharmacology. This assay measures an essential pathway in GPCR activation, i.e. β-arrestin recruitment to activated GPCRs, enabling scientists...
Unique Properties of PathHunter® β-Arrestin Assays for GPCR Antagonist Discovery and Characterization

A common feature of 7TM receptors is that upon activation, the receptors are bound by cellular Arrestin proteins. DiscoveRx has pioneered the PathHunter^® β-Arrestin assay platform for monitoring these events using enzyme fragment complementation (EFC) and applied this technique to develop assays for more than 170 human GPCR targets. Unlike second messenger assays that are am...
Using DiscoverX’s ADP QuestTM for Academic Screening of Novel Kinases
Enabling Functional Therapeutic Antibody Research Using PathHunter® β-Arrestin Technology
Evaluation of a New Intracellular Calcium Fluorescent Reagent Using the FDSS6000
Rapid Quantification of Bioactive Ligands in Serum and Human Plasma Using PathHunter® eXpress β-Arrestin GPCR Assays
[User Manual] HitHunter® cGMP Assay

The HitHunter^® cGMP assay measures cGMP in cell lysates from cells induced in suspension in a microtiter plate.
To B or Not To B: Phenotypic Profiling BTK Inhibitors in BioMAP® Systems

Screening compounds in primary human cell BioMAP® systems designed to model diseased tissues reinstates a more physiological approach to drug discovery. Here, we present BioMAP® analysis of two BTK inhibitors revealing cell-selectivity, efficacy and safety related activities. Ibrutinib is broadly active on endothelial, epithelial, smooth muscle cells and fibroblast-based systems, while ...
[DiscoverX/SGC Technology Symposium] - Selective Targeting of Protein Interactions Mediated by Epigenetic Effector Domains
[DiscoverX/SGC Technology Symposium] - Assays and Probes for Epigenetic Targets
[DiscoverX/SGC Technology Symposium] - Targeting Bromodomains – BET and the wider target class
[DiscoverX/SGC Technology Symposium] - Integrated Solution for Epigenetic Drug Discovery and Development
[DiscoverX/SGC Technology Symposium] - Application of computational approaches to accelerate bromodomain drug discovery
[User Manual] PathHunter® Pharmacotrafficking Assays

PathHunter Pharmacotrafficking cell lines are based on the enzymatic fragment complementation technology. The cells are expressed as a ProLink™ (PK)-tagged mutant transmembrane protein that is retained in the endoplasmic reticulum (ER) d...
[User Manual] PathHunter® Insulin Glargine Bioassay Kit

PathHunter^® Insulin Glargine Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study insulin glargine potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, diluti...
[User Manual] KILR® Detection Kit

KILR Detection Kit is to be used with the KILR Assays for Adherent or Suspension Cell Lines when running ADCC or other immune assays that result in cell lysis. The kit is easy-to-use and has been successfully run in 96-well microplate format. The resulting signal is chemiluminescent and is read with any standard plate reader.
[User Manual] PathHunter® Insulin Bioassay Kit

PathHunter^® Insulin Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study insulin potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, dilution buffer, and ass...
[User Manual] cAMP Hunter™ Exendin-4 Bioassay Kit

The cAMP Hunter Exendin-4 Bioassay Kits provide a robust, highly sensitive and easy-to-use assay for monitoring glucagon like peptide receptor 1 (GLP1R) activation based on 3'-5'-cyclic adenosine monophosphate (cAMP) production in cells.
[2016 Biopharmaceutical Symposium] Rapidly Develop Simple Potency Assays for Interleukins & Their Receptors

Ligand-induced receptor dimerization is an early functional step in receptor activation, representing the most proximal, functional read-out for Interleukin receptors. It is well understood that the family of Interleukin receptors will dimerize with the other members of its family leading to a complicated signaling cascade that is critically involved in a var...
[User Manual] InCELL Pulse™ Target Engagement Starter Kit

The InCELL Pulse Target Engagement Starter Kit provides reagents and protocols for the design and development of InCELL Pulse assays for the measurement of inhibitor cellular potency against user-defined protein targets of interest. The assay applies DiscoverX’s proprietary enzyme fragment complementation (EFC) technology to measure ligand dependent therm...
[User Manual] PathHunter® FGFR4-Beta-Klotho Bioassay Kit

PathHunter® FGFR4-Beta-Klotho Bioassay kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study FGF-19 potency and neutralizing antibodies. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, dilution buffer, and assay...
[User Manual] PathHunter® CHO-K1 VIPR2 Bioassay Kit

PathHunter CHO-K1 VIPR2 Bioassay Kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study drug potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qualified, ...
[User Manual] PathHunter® Pertuzumab Bioassay Kit

PathHunter Pertuzumab Bioassay kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study pertuzumab potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qualifi...
[User Manual] cAMP Hunter™ Liraglutide Bioassay Kit

cAMP Hunter Liraglutide Bioassay Kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study Liraglutide potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qual...
[User Manual] KILR® CD16 Effector Cells

KILR CD16 Effector Cells are purified human cytotoxic T lymphocytes stably expressing CD16 (FcγRIIIa; V158 variant), produced in a standardized batch. The cells were developed for Antibody-Dependent Cell-Mediated Cytotoxicity (ADCC) and T Cell Redirection (TCR) applications to reproducibly mediate target cell death.
[User Manual] PathHunter® U2OS MC4R Bioassay Kit

PathHunter U2OS MC4R Bioassay Kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study drug potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qualified, fro...
[User Manual] PathHunter® IL6R/IL6ST Bioassay Kit

PathHunter IL6R/IL6ST Bioassay kits provide a robust, highly sensitive, and easy-to-use cell-based functional assay to study potency of anti-IL-6R or anti-IL-6 antibodies and their neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, a...
[User Manual] PathHunter® Anakinra Bioassay Kit

PathHunter Anakinra Bioassay kits provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study anakinra potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-qualified, ...
[User Manual] PathHunter® PD-1 Signaling Bioassay Kit

For Chemiluminescent Detection of PD-L1-Induced PD-1 Signaling
[User Manual] PathHunter® Sargramostim Bioassay Kit

For Chemiluminescent Detection of Sargramostim Activity
[User Manual] InCELL Hunter™ Target Engagement Cell Lines
[User Manual] PathHunter® Checkpoint Assay - TNF Receptor Superfamily (TNFRSF)

The PathHunter Checkpoint Signaling Assay for Tumor Necrosis Factor Receptor Superfamily (TNFRSF) members (or receptors) is a simple, highly specific assay to enable discovery and development of small molecule and biologic drugs targeting the TNFR superfamily of receptors that activate the non-canonical NF-kB pathway through NF-kB inducing kinase (NIK). The assay is a robust measurement of co-s...
[User Manual] PathHunter® IL17RA/IL17RC Dimerization Bioassay Kit

PathHunter IL17RA/IL17RC Bioassay Kits provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study receptorreceptor interactions at the cell surface. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-validated, frozen bioassay cells hav...
[User Manual] PathHunter® Tocilizumab Bioassay Kit
[User Manual] cAMP Hunter™ NPY2R Bioassay Kit

The cAMP Hunter NPY2R Bioassay kits provide a robust, highly sensitive and easy-to-use assay for monitoring peptide YY activation based on 3'-5'-cyclic adenosine monophosphate (cAMP) production in cells..
[User Manual] PathHunter® CHO-K1 CNR1 Bioassay Kit
[User Manual] PathHunter® Jurkat SIRPα Signaling Bioassay Kit

The PathHunter SIRPα Signaling Bioassay Kit provides a simple, highly specific assay to enable discovery and development of small molecule and biologic drugs targeting the CD47-SIRPα signaling axis. The bioassay kit contains all the materials needed for a complete assay, including cells, detection reagents, cell plating reagent, positive control antibody, and assay plates. The cryop...
[User Manual] PathHunter® CHO-K1 BDKRB2 Bioassay Kit
[User Manual] PathHunter® U2OS IL31RA/OSMRb Dimerization Bioassay Kit
[User Manual] PathHunter® CHO-K1 AGTRL1 Bioassay Kit
[User Manual] PathHunter® Signaling Pathway Reporter Assay
[User Manual] PathHunter® CHO-K1 GLP2R Bioassay Kit
[User Manual] PathHunter® U2OS IL-10RA/IL-10RB Dimerization Bioassay Kit
[User Manual] PathHunter® CHO-K1 AGTR1 Bioassay Kit
[User Manual] cAMP Hunter™ CHO-K1 GPBAR1 Bioassay Kit
[User Manual] cAMP Hunter™CHO-K1 LHCGR Bioassay Kit
[User Manual] PathHunter® CHO-K1 AGTR1 Bioassay Kit
[User Manual] PathHunter® Adalimumab Bioassay Kit
[User Manual] PathHunter® U2OS GHSR Bioassay Kit
[User Manual] PathHunter®CHO-K1 MRGPRX2 Bioassay Kit
[User Manual] PathHunter® U2OS MCHR1 Bioassay Kit
[User Manual] ADP Quest™ Assay (90-0071 series)

The ADP Quest™ Assay is a biochemical assay to measure the accumulation of ADP, a product of kinase and ATPase enzyme activity. The Assay is useful for determining substrate Michaelis-Menten kinetics and for profiling inhibitor potency and mode of action. It can be run in either an endpoint or kinetic mode and is compatible with both peptide substrates and whole proteins. The Assay is for...
[User Manual] ADP Hunter™ Assay (90-0083 series)

ADP Hunter™ Plus is a biochemical assay to measure the accumulation of ADP, a product of kinase enzyme activity. ADP Hunter Plus is specifically designed for high throughput screening of kinase inhibitors, and is compatible with both peptide substrates and whole proteins. The assay has been designed for research use in 384-well microplates, but can also be run in additional microplate for...
[User Manual] PathHunter® TrkA-p75 Bioassay Kit

The PathHunter TrkA-p75 Bioassay kit provides a robust, highly sensitive, and easy-to-use functional cell based assay to study drug potency and neutralizing antibodies. The bioassay kit contains all the materials needed for a complete assay, including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The cryopreserved cells have been manufactured to en...
[User Manual] PathHunter® Internalization Assays

PathHunter Internalization Assays are cell-based assays that measure internalization of single-pass membrane receptors, e.g. receptor tyrosine kinases (ErbB-2), immune checkpoint receptors (CD33), mediated by small molecule or biologic therapeutics. Measuring drug-mediated receptor internalization can provide insight into diseases, drug tolerance, unwanted side effects and helps in identifying ...
[User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines

The ChemiSCREEN and ChemiBRITE Cell Lines are designed to enable the measurement of intracellular calcium levels when a GPCR of interest has been activated by a ligand. These cell lines are suitable for studying small molecules as well as biologics. The assay protocol has been optimized for use in either a 384-well or 96-well format.

ChemiSCREEN and ChemiBRITE cells stably expres...
[User Manual] InCELL Hunter™ eXpress Assays

InCELL Hunter™ eXpress Assays provide a cell-based approach to evaluate changes in protein stability upon compound binding. These assay kits have been validated for use in 96-well and 384-well microplate formats. The eXpress kits contain all the materials needed for a complete assay including cells, cell plating reagents, detection reagents, and plates. The pre-validated, cryopreserved eX...
[User Manual] PrecisION® Ion Channel Cell Lines

PrecisION cell lines are designed to provide pharmacologically-relevant cell models for research and screening applications.
[User Manual] SPRINTer™ Endogenous Protein Turnover Biosensor Cell Lines

SPRINTer Endogenous Protein Turnover Biosensor Cell Lines are stable clonal cell lines used for monitoring drug-induced protein turnover of a specific endogenous target. Genome engineering or editing techniques, such as CRISPR/Cas9, are used to introduce a small tag into the endogenous locus of interest. This allows for the quantitation of changes in target protein levels when cells are treated...
[User Manual] PathHunter® Aflibercept Bioassay HS Kit

PathHunter Aflibercept Bioassay HS Kit delivers a robust, highly sensitive, and easy-to-use functional cell-based assay to determine Aflibercept drug potency and detect neutralizing antibodies. This bioassay HS kit has been optimized further to deliver reproducible results with lower variability. The bioassay kit contains all the materials needed for a complete assay, including cryopreserved ce...
[User Manual] PathHunter® Bevacizumab Bioassay HS Kit

PathHunter® Bevacizumab Bioassay HS Kit provide a robust, highly sensitive and easy-to-use, cell-based functional assay to study bevacizumab potency and neutralizing antibodies. The Bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-validated, frozen cells have been...
[User Manual] PathHunter® Ranibizumab Bioassay HS Kit

PathHunter Ranibizumab Bioassay HS Kit provide a functional, robust, highly sensitive, and easy-to-use cell-based assay to study ranibizumab potency and neutralizing antibodies. The bioassay kits contain all the reagents needed for a complete assay including cells, detection reagents, cell plating reagent, positive control agonist, and assay plates. The pre-validated, frozen cells have been man...